Nanostructured liposome vector with highly effective antineoplastic activity

A nano-structured lipid, anti-tumor activity technology, applied in the direction of anti-tumor drugs, liposome delivery, organic active ingredients, etc., to achieve the effect of increasing uptake, improving curative effect, and reducing toxic and side effects

Inactive Publication Date: 2007-08-08
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Nanostructured liposome vector with highly effective antineoplastic activity
  • Nanostructured liposome vector with highly effective antineoplastic activity

Examples

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Embodiment 1

[0016] Example 1: Preparation and application of a monoglyceride nanostructured carrier loaded with paclitaxel containing 5% oleic acid

[0017] 1) Preparation of paclitaxel-loaded monoglyceride nanostructure carrier containing 5% oleic acid

[0018] Accurately weigh 30mg of lipid material (ratio of oleic acid to monoglyceride: 0.5 / 9.5) and 1.5mg of paclitaxel respectively, put them in 3mL of absolute ethanol, and dissolve them in a water bath at 70°C. With distilled water as the dispersed phase, put it in a 70°C water bath. At 400r·min -1 Under the condition of mechanical stirring, the organic phase was injected into 30 mL of the dispersed phase, and stirred for 5 min to obtain a monoglyceride nanostructured lipid carrier dispersion liquid with 5% oleic acid content. The resulting nanostructured lipid carrier dispersion was mixed with 3mol L -1 HCl solution to adjust the pH to 1.2, at 20000r·min -1 Centrifuge for 10 min, add 0.1% Poloxamer (w / v) to the precipitate to redi...

Embodiment 2

[0034] Example 2: Preparation and application of a monoglyceride nanostructured carrier loaded with paclitaxel containing 10% oleic acid

[0035] 1) Preparation of paclitaxel-loaded monoglyceride nanostructure carrier containing 10% oleic acid

[0036] Accurately weigh 30 mg of lipid material (ratio of oleic acid to monoglyceride: 1 / 9) and 1.5 mg of paclitaxel respectively, place in 3 mL of absolute ethanol, and dissolve in a water bath at 70°C. With distilled water as the dispersed phase, put it in a 70°C water bath. At 400r·min -1 Under the condition of mechanical stirring, the organic phase was injected into 30 mL of the dispersed phase, and stirred for 5 min to obtain a monoglyceride nanostructured lipid carrier dispersion liquid with 10% oleic acid content. The resulting nanostructured lipid carrier dispersion was mixed with 3mol L -1 HCl solution to adjust the pH to 1.2, at 20000r·min -1 Centrifuge for 10 min, add 0.1% Poloxamer (w / v) to the precipitate to redisperse...

Embodiment 3

[0046] Example 3: Preparation and application of a monoglyceride nanostructure carrier loaded with paclitaxel containing 20% ​​oleic acid

[0047] 1) Preparation of paclitaxel-loaded monoglyceride nanostructure carrier containing 20% ​​oleic acid

[0048] Accurately weigh 30 mg of lipid material (ratio of oleic acid to monoglyceride: 2 / 8) and 1.5 mg of paclitaxel respectively, place them in 3 mL of absolute ethanol, and dissolve in a water bath at 70°C. With distilled water as the dispersed phase, put it in a 70°C water bath. At 400r·min -1 Under the condition of mechanical stirring, the organic phase was injected into 30 mL of the dispersed phase, and stirred for 5 min to obtain a monoglyceride nanostructured lipid carrier dispersion liquid with 20% oleic acid content. The resulting nanostructured lipid carrier dispersion was mixed with 3mol L -1 HCl solution to adjust the pH to 1.2, at 20000r·min -1 Centrifuge for 10 min, add 0.1% Poloxamer (w / v) to the precipitate to re...

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Abstract

The invention relates to a nanometer liposome carrier with high-effect anti-tumor activity, which carries the anti-tumor Paclitaxel, while the liposome is formed by single lipid and liquid lipid, wherein, the liquid lipid is 5-20% of liposome, the Paclitaxel is 3.1-3.6% of solid liposome nanometer particles, and the diameter is 481-532nm. The invention has high-effect cell extraction and cell-pulp hold function via the nanometer liposome carrier, while the package on the anti-tumor drug whose molecule target is at the cell pulp can improve the adsorption of anti-tumor drug and improve the drug density at target part. The invention can improve the drug adsorption of tumor cell, reduce the drug distribution at normal cell, reduce the side effect and toxicity, and improve the effect.

Description

technical field [0001] The invention relates to the preparation of a nano-structured lipid carrier and the application of the nano-structured lipid carrier in antitumor therapy. Background technique [0002] Tumor has always been a major disease that directly threatens human health. Due to the lack of molecular targeting of the drug itself, tumor chemotherapy has major treatment problems such as low cure rate and huge toxic side effects. Directly targeting drugs to diseased tissues (organs), cells, and subcellular organelles through appropriate carrier technology is one of the important means to solve the low cure rate and toxic side effects of cancer chemotherapy. At present, scientists at home and abroad have made some progress in the tissue (organ) and cell targeting of tumor drugs through carrier technology, but have not achieved breakthrough efficacy. The essence is that the molecular targets of most anti-tumor drugs are located in cells. Therefore, the research and de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/12A61K31/337A61P35/00
Inventor 胡富强杜永忠袁弘游剑
Owner ZHEJIANG UNIV
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